More information about Gliclazide
Pronunciation(GLYE kla zide)
Generic AvailableYes: 80 mg tablet
Canadian Brand NamesApo-Gliclazide®; Diamicron®; Diamicron® MR; Novo-Gliclazide
UseManagement of type 2 diabetes mellitus (noninsulin dependent, NIDDM)
RestrictionsNot available in U.S.
Pregnancy Risk FactorNot available (similar agents rated C); manufacturer contraindicates use
Pregnancy ImplicationsClinical effects on the fetus: Crosses the placenta. Hypoglycemia; ear defects reported with sulfonylureas; other malformations reported but may have been secondary to poor maternal glucose control/diabetes. Insulin is the drug of choice for the control of diabetes mellitus during pregnancy.
LactationExcretion in breast milk unknown/contraindicated
ContraindicationsHypersensitivity to gliclazide, sulfonylureas, or any component of the formulation; type 1 diabetes mellitus (insulin dependent, IDDM), diabetic ketoacidosis with or without coma; renal or hepatic impairment; pregnancy (per manufacturer); breast-feeding
Warnings/PrecautionsAll sulfonylurea drugs are capable of producing severe hypoglycemia. Hypoglycemia is more likely to occur when caloric intake is deficient, after severe or prolonged exercise, when ethanol is ingested, or when more than one glucose-lowering drug is used. Hypoglycemia is also more likely in elderly patients, or in impaired renal or hepatic function.
Chemical similarities are present among sulfonamides, sulfonylureas, carbonic anhydrase inhibitors, thiazides, and loop diuretics (except ethacrynic acid). Use in patients with sulfonamide allergy is specifically contraindicated in product labeling, however, a risk of cross-reaction exists in patients with allergy to any of these compounds; avoid use when previous reaction has been severe. Safety and efficacy have not been established in pediatric patients.
Product labeling of sulfonylureas (in U.S.) states oral hypoglycemic drugs may be associated with an increased cardiovascular mortality as compared to treatment with diet alone or diet plus insulin. Data to support this association are limited, and several studies, including a large prospective trial (UKPDS), have not supported an association.
Adverse ReactionsFrequency not defined.
Central nervous system: Headache, nervousness, dizziness
Dermatologic: Rash, erythema, pruritus, urticaria. Sulfonylureas have also been associated with rare photosensitivity and porphyria cutanea tarda
Endocrine & metabolic: Hypoglycemia (dose dependent), hyponatremia (rare)
Gastrointestinal: Nausea, vomiting, diarrhea, epigastric fullness, gastritis
Hematologic: Agranulocytosis, leukopenia, thrombocytopenia, anemia
Hepatic: Jaundice, LDH increased, transaminases increased
Miscellaneous: Disulfiram reaction (very low potential)
Overdosage/ToxicologySymptoms of overdose include severe hypoglycemia, seizures, cerebral damage, tingling of lips and tongue, nausea, yawning, confusion, agitation, tachycardia, sweating, convulsions, stupor, and coma. Intoxication with sulfonylureas can cause hypoglycemia and is best managed with glucose administration (oral for milder hypoglycemia or by injection in more severe forms).
ACE inhibitors: May increase the hypoglycemic effect of gliclazide; monitor
Anabolic steroids: May increase hypoglycemic effect of gliclazide; monitor
Beta-blockers: Decrease hypoglycemic effect, mask most hypoglycemic symptoms, decrease glycogenolysis; avoid use in diabetics with frequent hypoglycemic episodes.
Corticosteroids: May cause hyperglycemia; adjustment of hypoglycemic agent may be necessary.
Cyclosporine: Gliclazide may increase serum concentrations of cyclosporine.
Fluoroquinolones: A possible interaction between sulfonylureas and fluoroquinolone antibiotics has been reported resulting in a potentiation of hypoglycemic action of sulfonylureas.
H2 antagonists, antacids, oral sodium bicarbonate: May increase the hypoglycemic effect; monitor glucose response.
Rifampin: May increase metabolism of gliclazide, decreasing its effects.
Salicylates: May increase hypoglycemic effect of gliclazide.
Sulfonamides: May increase hypoglycemic effect of gliclazide.
Thiazide diuretics: Hypoglycemic effect of gliclazide may be decreased by thiazide diuretics.
Warfarin: Anticoagulant effects may be increased by sulfonylureas.
Ethanol: Avoid ethanol (may cause hypoglycemia and/or rare disulfiram reactions).
Herb/Nutraceutical: Avoid chromium, garlic, gymnema (may cause hypoglycemia).
StabilityStore at 20°C to 30°C (68°F to 86°F).
Mechanism of ActionStimulates insulin release from the pancreatic beta cells; reduces glucose output from the liver; lowers plasma glucose concentrations. Gliclazide has also been shown to decrease platelet aggregation at therapeutic doses.
Protein binding: 94%
Metabolism: Hepatic, to inactive metabolites
Half-life elimination: 10 hours
Time to peak: 4-6 hours
Excretion: Urine (60% to 70%) and feces (10% to 20%) as metabolites
Immediate release tablet: Initial: 80-160 mg/day; typical dose range 80-320 mg/day; dosage of
Sustained release tablet: 30-120 mg once daily
Note: There is no fixed dosage regimen for the management of diabetes mellitus with gliclazide or any other hypoglycemic agent. Dose must be individualized based on frequent determinations of blood glucose during dose titration and throughout maintenance.
Dosage adjustment in renal/hepatic impairment: Contraindicated in severe impairment
AdministrationPatients who are anorexic or NPO, may need to have their dose held to avoid hypoglycemia. Should be administered with meals.
Monitoring ParametersSigns and symptoms of hypoglycemia, fasting blood glucose, hemoglobin A1c
Reference RangeTarget range: Adults:
Fasting blood glucose: <120 mg/dL
Glycosylated hemoglobin: <7%
Dietary ConsiderationsShould be taken with meals. Dietary modification based on ADA recommendations is a part of therapy. Decreases blood glucose concentration. Hypoglycemia may occur. Must be able to recognize symptoms of hypoglycemia (palpitations, sweaty palms, lightheadedness).
Patient EducationThis medication is used to control diabetes; it is not a cure. Other components of treatment plan are important: follow prescribed diet, medication, and exercise regimen. Take exactly as directed; with meal(s) at the same time each day. Do not change dose or discontinue without consulting prescriber. Avoid alcohol while taking this medication; could cause severe reaction. Inform prescriber of all other prescription or OTC medications you are taking; do not introduce new medication without consulting prescriber. Do not take other medication within 2 hours of this medication unless advised by prescriber. If you experience hypoglycemic reaction, contact prescriber immediately. Maintain regular dietary intake and exercise routine and always carry quick source of sugar with you. You may be more sensitive to sunlight (use sunscreen, wear protective clothing and eyewear, and avoid direct sunlight). You may experience side effects during first weeks of therapy (headache, nausea); consult prescriber if these persist. Report severe or persistent side effects, extended vomiting or flu-like symptoms, skin rash, easy bruising or bleeding, or change in color of urine or stool. Pregnancy/breast-feeding precautions: Inform prescriber if you are or intend to become pregnant. Do not breast-feed.
Additional InformationNot available in U.S.
Cardiovascular ConsiderationsThe possibility of higher doses of sulfonylureas eliciting an increase in cardiovascular events, because of their effects on blocking potassium sensitive ATP channels, has been raised. However, there are presently only limited data to support this premise, particularly with newer generation agents. An early study suggested poor cardiovascular outcomes in diabetic patients treated with tolbutamide. Retrospective studies evaluating cardiovascular outcomes following angioplasty and acute myocardial infarction in diabetic patients receiving newer sulfonylureas are inconsistent. Longer-term prospective trials of sulfonylurea therapy, such as the UKPDS, do not reveal any increased cardiovascular mortality.
Dental Health: Effects on Dental TreatmentNo significant effects or complications reported
Dental Health: Vasoconstrictor/Local Anesthetic PrecautionsNo information available to require special precautions
Mental Health: Effects on Mental StatusMay cause nervousness and dizziness
Mental Health: Effects on Psychiatric TreatmentMay cause leukopenia, thrombocytopenia, and agranulocytosis; use caution with clozapine, carbamazepine, and valproic acid
Tablet (Diamicron®): 80 mg
Tablet, sustained release (Diamicron® MR): 30 mg
International Brand NamesAglucide® (AR); Apo-Gliclazide® (CA, NZ); Betanorm® (TR); Cadicon® (TH); Comprid® (BD); Diabeside® (TH); Diabest® (RU); Diabeton® (RU); Diabezidum® (PL); Diabrezide® (AT, IE, IT, PL, RO); Diaclide® (IE); Diactin® (BD); Diaglyk® (GB); Diaklat® (PL); Diamaze® (TH); Diamexon® (TH); Diamicron® (AR, AT, AU, BE, BR, CA, CH, CO, CR, CZ, DE, DK, DO, EG, ES, FR, GB, GT, HK, HN, ID, IE, IN, IT, JO, KW, LB, LU, MT, NL, NZ, PA, PT, SG, SV, SY, TH, TR, ZA); Diamicron® MR (CA); Dianid® (TH); Diaprel® (CZ, HR, HU, PL, RO, SI, YU); Diatrol® (BD); Diazidan® (PL); Glibet® (ID); Glicab® (ID); Gliclazida® (BR, CO); Gliclazida Irex® (PT); Gliclazide Alpharma ApS® (SG); Gliclazide Edmond® (IT); Gliclazide® (GB, PL, RU); Gliclazide Molteni® (IT); Gliclazide Teva® (IT); Glicron® (TH); Glidabet® (ID); Glidiet® (RO); Glikamel® (ID); Gliklazyd® (PL); Glikosan® (YU); Glimicron® (JP, SG); Glinormax® (PL); Glioral® (YU); Glipicrone® (RO); Glizid® (BD); Glucocron® (TH); Glucodex® (ID); Glucozid® (BD); Glucozide® (SG); Gluctam® (HU, PL); Glumeco® (ID); Glumikron® (TR); Glyade® (AU); Glycafor® (ID); Glycon® (TH); Glygard® (ZA); Gored® (BD, ID); Lycazid® (IN); Medoclazide® (RO, SG, TH); Melicron® (SG); Melizide® (SG); Merck-Gliclazide® (BE); Norsulin® (PL); Novo-Gliclazide (CA); Nufamicron® (ID); Oramikron® (TR); Pedab® (ID); Predian® (RU, YU); S.C.D. Glyclazide® (SG); Serviclazide® (TH); Tiaglib® (ID); Unava® (AR); Uni Diamicron® (BE); Xepabet® (ID); Zibet® (ID); Ziclin® (ZA); Zumadiac® (ID); Zumamet® (ID)